Formestane, 4-Hydroxyandrostenedione, CGP-32349, 4-OHA, Lentaron Depot, Lentaron-药物合成数据库

【药物名称】Formestane, 4-Hydroxyandrostenedione, CGP-32349, 4-OHA, Lentaron Depot, Lentaron

化学结构式(Chemical Structure):

参考文献No.	374223
标题:	Novel approach to the synthesis of the aromatase inhibitor 4-hydroxyandrost-4-ene-3,17-dione (4-OHA)
作者:	Melo, M.L.S.E.; Neves, A.S.C.; da Silva, E.J.T.
来源:	J Chem Soc - Perkins Trans I 1996,14(14),1649

合成路线图解说明: A novel synthetic strategy for the preparation of formestane has been published: The oxidation of 5alpha-3-androsten-17-one (I) with H2O2 in formic acid gives the epoxide (II), which, without isolation, yields 3alpha,4beta-dihydroxy-5alpha-androstan-17-one (III). The reaction of (III) with DMSO and trifluoroacetic anhydride (TFAA), and then with triethylamine affords 3-hydroxy-5alpha-2-androstene-4,17-dione (IV), which is finally submitted to basic isomerization catalyzed by sodium methoxide